SINGLE-DOSE BIOAVAILABILITY OF ORAL AND INTRAMUSCULAR THIOCOLCHICOSIDE IN HEALTHY-VOLUNTEERS

A single dose of 8 mg of thiocolchicoside was administered to 12 healt hy volunteers according to a Latin square design, either as tablets (r eference), oral solution, or intramuscular injection. Serum thiocolchi coside concentrations showed an absorption phase followed by a biexpon ential decay with a terminal half-life (t(1/2)beta) of approximately 5 h, similar for the three formulations. The relative bioavailability o f both oral formulations was approximately 25%, compared to the intram uscular formulation. There was a trend for the oral solution to have a slightly larger AUC and C-max, as well as a slightly shorter T-max, t han the tablet formulation. However, the comparison of the two oral fo rms did not show statistically significant differences in the pharmaco kinetic parameters C-max, T-max, and AUC, suggesting that the Coltramy l(R) tablets have an adequate in vivo dissolution profile.